摘要:
The present invention provides a new process and intermediates for the production of antiviral compound 4′,4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2′-disulfonic acid and its pharmaceutically acceptable salts.
摘要:
The present invention provides a new process and intermediates for the production of antiviral compound 4′,4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2′-disulfonic acid and its pharmaceutically acceptable salts.
摘要:
The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.
摘要:
The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, selected from H; C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently selected from H, halogen, --NO.sub.2, alkyl, alkoxy, C.sub.1 -C.sub.6 perfluorinated alkyl, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, --CN, --O--R.sup.1, --O--Ar, --S--R.sup.1, --S--Ar, --SO--R.sup.1, --SO--Ar, --SO.sub.2 --R.sup.1, --SO.sub.2 --Ar, --CO--R.sup.1, --CO--Ar, --CO.sub.2 --R.sup.1, or --CO.sub.2 --Ar; and Y is selected from a) the moiety: ##STR2## wherein R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.n --.
摘要:
The present invention provides a new process and intermediates for the production of antiviral compound 4′,4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2′-disulfonic acid and its pharmaceutically acceptable salts.
摘要:
The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is 0 or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.
摘要:
The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.
摘要:
The present invention provides processes for the purification of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol. The processes include recrystallizing the compound from a solution comprising acetone and acetonitrile; treating the crude purified product with a clarifying agent in a solution comprising ethyl acetate, and precipitating or triturating the compound from a mixed solvent system.
摘要:
The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.